KR940021533A - 벤즈이미다졸 화합물, 그들의 용도 및 제조방법 - Google Patents

벤즈이미다졸 화합물, 그들의 용도 및 제조방법 Download PDF

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KR940021533A
KR940021533A KR1019940005924A KR19940005924A KR940021533A KR 940021533 A KR940021533 A KR 940021533A KR 1019940005924 A KR1019940005924 A KR 1019940005924A KR 19940005924 A KR19940005924 A KR 19940005924A KR 940021533 A KR940021533 A KR 940021533A
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phenyl
benzimidazole
pyridyl
alkyl
imidazolyl
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KR100297444B1 (ko
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엑셀쏜 오스카
튜버 레네
웨트젠 프랭크
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피터 울프
뉴로서치 에이/에스
사사이 아키라
메이지 세이카 가부시키가이샤
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Abstract

본 특허출원은 다음 구조식을 갖는 화합물 또는 그들의 제약학적으로 허용가능한 염을 나타낸다.
(여기서, R3, R4, R6 및 R7은 상기한 바와 동일하다.) 화합물은 간질 및 다른 경련 장해, 불안, 불면증 및 기억장해와 같은 여러 가지 중추신경계 장해의 치료를 위해 사용한다.

Description

벤즈이미다졸 화합물, 그들의 용도 및 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 다음식을 갖는 화합물 또는 제약학적으로 허용 가능한 그들의 염.
    위식에서, R3는
    (위식에서, X는 N; 또는 C-R′이고, 여기서 R′는 수소 또는 R4와 함께 -(NR111)m-C(=O)-, -(NR111)m-C(=O)-, 또는 -N=C- 가교를 형성하고, 여기서 R111은 수소 또는 알킬이고, m은 0 또는 1이고; A, B, C 및 D중의 하나는 N이고, 다른 것은 CH이고; E, F, G 및 K중의 하나는 N-R″이고, 여기서 R″는 수소 또는 알킬이고, E, F, G 및 K중 다른 것은 CH2이다.)이고, R6및 R7은 독립적으로 수소; 할로겐; 아미노; 니트로; 시아노; 아실아미노; 트리플루오로메틸; 알킬; 알콕시; COO-알킬; 아실; CH=NOH, CH=NO-알킬; CH-N-NH-(C=O)-NH2; 알킬, 니트로, 할로겐, 또는 CF3로 한번 또는 그 이상을 치환시킬 수 있는 페닐; 또는 알킬, 페닐, 할로겐 또는 CF3로 한번 또는 그 이상을 치환시킬 수 있는 아릴; 또는 R6및 R3과 함께 (CH2)a-(Z)b-(C=Y)c-(Z′)D-(CH2)e 가교를 형성하고, 여기서 Z 및 Z′는 각각 독립적으로 O, S 또는 NR″′이고, 여기서 R″′는 수소 또는 알킬이고, Y는 O 또는 H2, a 및 e는 각각 독립적으로 0, 1, 2 또는 3이고 b, c 및 d는 각각 독립적으로 0 또는 1이고 a, b, c, d 및 e의 합은 6을 초과하지 않고, R6및 R7과 함께 -CH-CH-CH=N-, -CH=CH-N=CH-, -CH=N-CH=CH-, -N=CH-CH=CH-, 또는 =N-S-N= 가교를 형성하고, R4는 수소; 아미노; 니트로; 시아노; 할로겐; 아실아미노; 알킬, 아미노, 할로겐, 또는 CF3로 한번 또는 그 이상을 치환시킬 수 있는 페닐; 또는 알킬, 페닐, 할로겐 또는 CF3로 한번 또는 그 이상을 치환시킬 수 있는 아릴; 또는 R′와 함께 R÷는 -(NR111)m-C(=O)-, -(NR111)m-CHOH-, 또는 -N=C- 가교를 형성하고, 여기서 R111은 수소 또는 알킬이고, m은 1이고; R11은 알킬, 할로겐 또는 CF3로 한번 또는 그 이상을 치환시킬 수 있는 페닐; 또는 알킬, 할로겐 또는 CF3로 한번 또는 그 이상을 치환시킬 수 있는 벤즈이미다졸릴; 또는 알킬, 페닐, 할로겐 또는 CF3, 아미노, 니트로, 시아노, 아실아미노, 트리플루오로메틸로 한번 또는 그 이상을 치환시킬 수 있는 아릴; 알콕시; 또는 아실이고, R6및 또는 그 이상 치환시킬 수 있는 아릴; 알콕시; 또는 아실이고, R6및 R7의 적어도 하나는 수소 이외의 것이다.
  2. 제1항에 있어서, 상기한 화합물에서 R4가 수소이고, R3는
    (여기서, R11은 피리딜이다.)인 화합물.
  3. 제1항에 있어서, 1-[3-(3-피리딜)-페닐]-5-메틸알독시모-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-i-프로필-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-(2-푸라닐)-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-6-이오도-벤즈이미다졸, 1-[3-(1-이미다졸릴)-페닐]-5-메틸-벤즈이미다졸, 1-[3-(1-이미다졸릴)-페닐]-5-t-부틸-벤즈이미다졸, 1-[3-(1-이미다졸릴)-페닐]-5-페닐-벤즈이미다졸, 1-[3-(1-이미다졸릴)-페닐]-5-i-프로필-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-이오도-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-t-부틸-벤즈이미다졸, 1-[3-(1-벤즈이미다졸릴)-페닐]-5-i-프로필-벤즈이미다졸, 1-[3-(1-(2-메틸이미다졸-페닐]-5-페닐-벤즈이미다졸, 1-[3-(1-벤즈이미다졸릴)-페닐]-5-트리플루오로메틸-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-(3-푸라닐)-벤즈이미다졸, 또는 4-트리플루오로메틸-6, 7-디히드로-6-메틸-7-옥소-벤즈이미다조-[3, 4-ab][1, 4]벤조디아제핀, 또는 제약학적으로 허용 가능한 그들의 염인 화합물.
  4. 적어도 하나의 제약학적으로 허용 가능한 기초제 또는 희석제와 함께. 제1항의 화합물 또는 그들의 제약학적으로 허용 가능한 첨가염의 효과적인 양으로 이루어진 제약학적인 조성물.
  5. 인간을 포함하는 살아있는 동물체와 같은 중추 신경계의 벤조디아제핀 수용체의 변형에 응답하는 인간을 포함하는 살아있는 동물체의 장해 또는 질병을 치료하기 위한 약제의 제조를 위한 제1항의 화합물의 용도.
  6. 인간을 포함하는 살아있는 동물체와 같은 중추 신경계의 벤조디아제핀 수용체의 변형에 응답하는 인간을 포함하는 살아있는 동물체의 장해 또는 질병을 치료하기 위한 약제의 제조를 위한 상기 제2항의 화합물의 용도.
  7. 인간을 포함하는 살아있는 동물체의 불안, 불면증, 기억장해, 간질 또는 어떤 다른 경련 장해의 치료를 위한 약제의 제조를 위한 제1항의 화합물의 용도.
  8. 제5항에 있어서, 사용된 화합물은 1-[3-(3-피리딜)-페닐]-5-메틸알독시모-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-i-프로필-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-(2-푸라닐)-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-6-이오도-벤즈이미다졸, 1-[3-(1-이미다졸릴)-페닐]-5-메틸-벤즈이미다졸, 1-[3-(1-이미다졸릴)-페닐]-5-t-부틸-벤즈이미다졸, 1-[3-(1-이미다졸릴)-페닐]-5-페닐-벤즈이미다졸, 1-[3-(1-이미다졸릴)-페닐]-5-i-프로필-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-이오도-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-t-부틸-벤즈이미다졸, 1-[3-(1-벤즈이미다졸릴)-페닐]-5-i-프로필-벤즈이미다졸, 1-[3-(1-(2-메틸이미다졸릴-페닐]-5-페닐-벤즈이미다졸, 1-[3-(1-벤즈이미다졸릴)-페닐]-5-트리플루오로메틸-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-(3-푸라닐)-벤즈이미다졸, 또는 4-트리플루오로메틸-6, 7-디히드로-6-메틸-7-옥소-벤즈이미다조-[3, 4-ab][1, 4]벤조디아제핀, 또는 그들의 제약학적으로 허용 가능한 첨가염인 용도.
  9. 포름산 또는 그들의 반응 유도체와 다음식을 갖는 화합물의 반응 단계로 이루어지는 제1항의 화합물의 제조방법.
    (위 식에서, R3, R4, R6 및 R7은 상기한 바와 같다.)
  10. 제9항에 있어서, 1-[3-(3-피리딜)-페닐]-5-메틸알독시모-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-i-프로필-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-(2-푸라닐)-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-6-이오도-벤즈이미다졸, 1-[3-(1-이미다졸릴)-페닐]-5-메틸-벤즈이미다졸, 1-[3-(1-이미다졸릴)-페닐]-5-t-부틸-벤즈이미다졸, 1-[3-(1-이미다졸릴)-페닐]-5-페닐-벤즈이미다졸, 1-[3-(1-이미다졸릴)-페닐]-5-i-프로필-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-이오도-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-t-부틸-벤즈이미다졸, 1-[3-(1-벤즈이미다졸릴)-페닐]-5-i-프로필-벤즈이미다졸, 1-[3-(1-(2-메틸이미다졸릴-페닐]-5-페닐-벤즈이미다졸, 1-[3-(1-벤즈이미다졸릴)-페닐]-5-트리플루오로메틸-벤즈이미다졸, 1-[3-(3-피리딜)-페닐]-5-(3-푸라닐)-벤즈이미다졸, 또는 4-트리플루오로메틸-6, 7-디히드로-6-메틸-7-옥소-벤즈이미다조-[3, 4-ab][1, 4]벤조디아제핀, 또는 그들의 제약학적으로 허용 가능한 첨가염인 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940005924A 1993-03-24 1994-03-24 벤즈이미다졸화합물,그들의용도및제조방법 KR100297444B1 (ko)

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